U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 41 - 50 of 261 results

Status:
Investigational
Source:
INN:naftalofos
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

The organophosphate compound Naftalofos is an anthelmintic drug. In Australia it is approved for veterinary use. Naftalofos has been used for many years to control nematodes of livestock. Naftalofos boluses are used against nematodes of cattle. Naphthalophos (36.6 to 51.2 mg/kg) was also 93% efficient against the multiple resistant strains of Trichostrongylus colubriformis in sheep. Naphthalophos showed efficacy against Haemonchus contortus (> 99 %),Trichostrongylus axei (99.3 %), Teladorsagia circumcincta (97.8 %), Trichostrongylus colubriformis (99.2 %), Cooperia punctata/curticei/pectinata (90.4 %), Nematodirus spathiger (89.2 %) and Oesophagostomum venulosum/columbianum (93.7 %). Naphthalophos represents an effective therapeutic alternative for incorporation into worm control programmes.
Status:
Investigational
Source:
INN:resorantel
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Resorantel (HOE 296V) is an anthelmintic agent. Resorantel was found to be highly effective against Houttuynia struthionis (a tapeworm, parasite of the small intestine) in ostriches. Resorantel also showed anthelmintic efficacy against Thysaniezia giardi and Avitellina spp. (both tapeworms) when tested in sheep. Similar results have been found in goats and cattle.
Status:
Investigational
Source:
INN:amidantel
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

N-(4-[(1-(Dimethylamino)-ethylidene)-amino]-phenyl)-2 methoxyacetamide hydrochloride (amidantel, BAY d 8815) is an aminophenylamidine with an interesting anthelminthic spectrum. In rodents the compound is active against nematodes, filariae and cestodes. Of special interest is the high efficacy in dogs against hookworms and large roundworms. Amidantel was well tolerated by all animals tested and did not show teratogenic effects. The drug was moderately potent inhibitor of both E. electricus and C. elegans acetylcholinesterase but at concentrations too high to account for its abilitiy to contract cut worms. The primary mode of action of amidantel appears to be as agonist at the level of the acetylcholine receptor, a view supported by the observation that its effect may be blocked by the nicotinic antagonists d-tubocurarine and gallamine. Amidantel was also investigated it clinical trials as the treatment against Ancylostoma duodenale infection. Amidantel proved to be very effective against A. duodenale as well as Ascaris lumbricoides. With regard to dosage, a single dose of 6.0 mg/kg body weight of amidantel was found to be the most effective and well tolerated than the other dosages employed.
Status:
Investigational
Source:
INN:nitramisole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nitramisole, an imidazothiazole derivative, is an anthelmintic. Nitramisole was effective against migrating Strongylus vulgaris larvae in ponies. Treatment of infected ponies with Nitramisole resulted both a clinical and radical cure.
Status:
Investigational
Source:
INN:nitrodan
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nitrodan is an anthelmintic drug. Nitrodan was effective when administered in feed against Hymenolepis nana and Syphacia obvelata infections in mice, Ascaridia galli infections in chickens, and Toxocara canis, Ancylostoma caninum, and Uncinaria stenocephala infections in dogs. This drug was not effective against Aspiculuris tetraptera, Nematospiroides dubius, and Nippostrongylus muris in mice or Toxascaris leonina in dogs. Long-term continuous feeding of 230 ppm nitrodan should provide an easy and efficient means of reducing infections of A. galli in chickens, and T. canis, A. caninum, and U. stenocephala in dogs, while minimizing opportunities for reexposure.
Status:
Investigational
Source:
INN:teroxalene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Teroxalene is a dioxopiperazine derivative with multidrug resistance reversal activity
Status:
Investigational
Source:
INN:vincofos
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Vincofos is a broad-spectrum canine anthelmintic. All or nearly all of the ascarids, hookworms, whipworms, and the tapeworm, Taenia pisiformis, were expelled following therapy with vincofos. The tapeworm, Dipylidium caninum, was also effectively removed by the vincofos treatment, but it appeared that a slightly greater dosage would be required to obtain maximum anthelmintic effect.
Status:
Investigational
Source:
USAN:Artemifone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Artemisone (also known as BAY-44-9585; BAY-449585) is a 10-amino-artemisinin derivative that is markedly superior in vitro and in vivo to current artemisinins against malaria and also possesses antitumor activity. Nonetheless, its low water solubility and bioavailability has limited its clinical use, that is why was studied the encapsulated artemisone against human melanoma A-375. In addition, artemisone has the potential to be efficacious for the treatment of H. pylori infection, especially in combination with antibiotics.
Status:
Investigational
Source:
INN:moxipraquine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Moxipraquine is alkylaminopiperazinyl derivative patented by Wellcome Foundation Ltd. as antiparasitic agent effective against Trypanosoma cruzi. Moxipraquine was effective in suppressing parasitaemia but did not eradicate the infection from mice or guinea-pigs. Moxipraquine was less potent against mouse infections with strain Peru than it was against other strains of T. cruzi. In limited tests, moxipraquine was effective on experimental infections of Leishmania major, L. mexicana mexicana and L. brasiliensis panamensis but not L.b. brasiliensis. Significant foetal toxicity, observed experimentally in rats and rabbits, resulted in the termination of further trials.
Hycanthone is a thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. It was clinically available for the treatment of human schistosomiasis. Anti-helmintic action relies on its ability to inhibit worm monoamine oxidase and cholinesterases. Hycanthone produced immediate side effects such as hepatotoxicity and gastrointestinal disturbances, and was consequently withdrawn. Hycanthone inhibits apurinic endonuclease-1 (APE1) by direct protein binding. Hycanthone was used in the 1980s as antitumor agents, it was pulled out of Phase II trials.